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Updated: Mar 8, 2026
Identification of Novel CK2 Kinase Substrates Using a Versatile Biochemical Approach
Published on: February 21, 2019
CK2 in Cancer: Cellular and Biochemical Mechanisms and Potential Therapeutic Target
Melissa M J Chua1, Charina E Ortega2, Ayesha Sheikh3
1Department of Medicine, School of Medicine, Boston University, Boston, MA 02118, USA. mel98791@bu.edu.
Abstract:
CK2 genes are overexpressed in many human cancers, and most often overexpression is associated with worse prognosis. Site-specific expression in mice leads to cancer development (e.g., breast, lymphoma) indicating the oncogenic nature of CK2. CK2 is involved in many key aspects of cancer including inhibition of apoptosis, modulation of signaling pathways, DNA damage response, and cell cycle regulation. A number of CK2 inhibitors are now available and have been shown to have activity against various cancers in vitro and in pre-clinical models. Some of these inhibitors are now undergoing exploration in clinical trials as well. In this review, we will examine some of the major cancers in which CK2 inhibition has promise based on in vitro and pre-clinical studies, the proposed cellular and signaling mechanisms of anti-cancer activity by CK2 inhibitors, and the current or recent clinical trials using CK2 inhibitors.
Insights
Protein kinase CK2 (CK2) is overexpressed in many cancers, driving tumor growth and progression. CK2 inhibitors show promise as anti-cancer therapeutics, with several agents in clinical trials for various malignancies.
Area of Science:
- Oncology
- Molecular Biology
- Biochemistry
Background:
- Protein kinase CK2 (CK2) is frequently overexpressed in human cancers.
- CK2 overexpression correlates with poor prognosis and contributes to oncogenesis.
- CK2 plays critical roles in cancer progression, including apoptosis inhibition, signaling pathway modulation, DNA damage response, and cell cycle regulation.
Purpose of the Study:
- To review the therapeutic potential of CK2 inhibitors in major human cancers.
- To elucidate the cellular and signaling mechanisms underlying CK2 inhibitor anti-cancer activity.
- To summarize the current status of CK2 inhibitors in clinical trials.
Main Methods:
- Literature review of in vitro and pre-clinical studies on CK2 inhibitors.
- Analysis of proposed mechanisms of action for CK2 inhibitors.
- Compilation of data from ongoing and recent clinical trials.
Main Results:
- CK2 inhibitors demonstrate anti-cancer activity in various cancer types in vitro and in pre-clinical models.
- CK2 inhibition impacts key cancer hallmarks such as apoptosis, signaling, DNA repair, and cell cycle.
- Several CK2 inhibitors are progressing through clinical trials for cancer treatment.
Conclusions:
- CK2 inhibition represents a promising therapeutic strategy for multiple human cancers.
- Understanding the mechanisms of CK2 inhibitors is crucial for optimizing their clinical application.
- Ongoing clinical trials will determine the efficacy and safety of CK2 inhibitors in cancer patients.
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